里程碑，雙特異性偶聯(lián)藥物獲批之后，“魔法子彈”還有哪些新可能？

編者按：偶聯(lián)藥物通過將抗體、多肽、小分子或其他靶向配體與功能性載荷連接，實現(xiàn)向特定細胞、組織或疾病微環(huán)境遞送治療載荷的效果。2026年第二季度，偶聯(lián)藥物領域延續(xù)了快速發(fā)展的態(tài)勢。多款抗體偶聯(lián)藥物（ADC）取得重要監(jiān)管進展，進一步走向一線治療、早期疾病管理和罕見腫瘤治療場景。首款雙特異性ADC獲批上市，并在三陰性乳腺癌和食管鱗狀細胞癌等適應癥中取得后期臨床積極結果，顯示雙抗原識別策略正在進入更成熟的臨床開發(fā)階段。與此同時，圍繞新型載荷、連接子、雙載荷ADC和抗體偶聯(lián)降解劑（DAC）的并購與合作持續(xù)活躍，放射性核素偶聯(lián)藥物（RDC）融資也在升溫，提示偶聯(lián)藥物的創(chuàng)新正在從傳統(tǒng)ADC進一步擴展到更廣泛的靶向遞送平臺。

在這一過程中，連接子與載荷是決定ADC能否從分子構想走向可開發(fā)候選藥物的關鍵因素之一。藥明康德研發(fā)化學服務部（Research Chemistry Services，RCS）構建了覆蓋連接子與載荷合成、分析及純化的一體化技術平臺，為ADC關鍵小分子組件開發(fā)提供系統(tǒng)化支持。依托超過10年的項目經(jīng)驗、580余名專業(yè)化學家團隊，以及包含1000余種連接子、30多類抗體連接位點和超過30種新型載荷及其類似物的可定制化體系，RCS能夠幫助合作伙伴高效推進ADC連接子與載荷開發(fā)，加速創(chuàng)新偶聯(lián)療法從早期研究邁向可開發(fā)階段。

ADC走向一線治療和早期疾病管理

2026年第二季度，多款ADC進一步進入一線治療和早期治療場景。5月，美國FDA批準阿斯利康（AstraZeneca）和第一三共（Daiichi Sankyo）聯(lián)合開發(fā)的Datroway（datopotamab deruxtecan）用于治療不可切除或轉移性三陰性乳腺癌（TNBC）成人患者，這些患者不適合接受PD-1/PD-L1抑制劑治療。Datroway是一款TROP2靶向ADC。

僅一個月后，另一款靶向TROP2的ADC也在一線TNBC治療中取得重要監(jiān)管進展。6月，美國FDA批準Trodelvy（sacituzumab govitecan）用于兩項TNBC一線適應癥：一是作為單藥用于不適合接受PD-1/PD-L1抑制劑治療的不可切除局部晚期或轉移性TNBC成人患者；二是與Keytruda（pembrolizumab）或Keytruda Qlex聯(lián)用，用于腫瘤PD-L1表達CPS≥10、適合接受免疫治療的不可切除局部晚期或轉移性TNBC成人患者。臨床試驗數(shù)據(jù)顯示，在ASCENT-03研究中，Trodelvy單藥組中位無進展生存期（PFS）為9.7個月，對照化療組為6.9個月；在ASCENT-04/KEYNOTE-D19研究中，Trodelvy聯(lián)合Keytruda組中位PFS為11.2個月，對照組為7.8個月。

Datroway和Trodelvy先后成為TNBC一線治療選擇，顯示ADC不再只是多線治療后的補充選擇，而正在與化療、免疫治療等標準方案共同影響一線治療決策。尤其是Trodelvy聯(lián)合Keytruda的獲批，也提示ADC與免疫檢查點抑制劑的聯(lián)合治療正在成為重要開發(fā)方向。ADC可通過靶向遞送細胞毒性載荷誘導腫瘤細胞死亡，而免疫治療則可激活抗腫瘤免疫反應，兩者聯(lián)用有望為部分患者帶來更深、更持久的疾病控制。

除了用于晚期癌癥一線治療外，ADC也在向早期疾病管理拓展。5月，Enhertu（trastuzumab deruxtecan）獲得美國FDA批準，用于HER2陽性早期乳腺癌的兩個新適應癥，包括作為新輔助療法和輔助療法，治療不同類型的早期HER2陽性乳腺癌患者。

這一進展具有重要意義。長期以來，ADC主要用于晚期、復發(fā)或難治性腫瘤患者；而當ADC進入新輔助和輔助治療場景，它的價值就不只是延緩晚期疾病進展，還可能參與早期疾病的根治性治療策略。

在罕見血液腫瘤領域，ADC也取得監(jiān)管進展。5月，美國FDA批準艾伯維（AbbVie）開發(fā)的Decnupaz（pivekimab sunirine）用于治療成人母細胞性漿細胞樣樹突狀細胞腫瘤（BPDCN）。Decnupaz是一款CD123靶向抗體偶聯(lián)藥物。

雙特異性ADC首次獲得監(jiān)管批準，臨床管線加速擴展

在ADC走向更廣泛臨床應用的同時，雙特異性ADC也在2026年第二季度迎來重要進展。6月，中國國家藥品監(jiān)督管理局（NMPA）批準百利天恒開發(fā)的倫康依隆妥單抗（izalontamab brengitecan）上市，用于治療復發(fā)或轉移性鼻咽癌患者。倫康依隆妥單抗同時靶向EGFR和HER3，是首款獲得監(jiān)管機構批準上市的雙特異性ADC。百時美施貴寶（Bristol Myers Squibb）已與百利天恒子公司SystImmune達成合作，共同開發(fā)這款藥物。

在2026年美國臨床腫瘤學會（ASCO）年會上，百時美施貴寶與百利天恒公布了iza-bren兩項3期臨床試驗的積極結果。在既往接受治療的不可切除局部晚期或轉移性TNBC患者中，PANKU-Breast02研究顯示，iza-bren較醫(yī)生選擇化療顯著改善總生存期（OS）和PFS；在復發(fā)或轉移性食管鱗狀細胞癌患者中，PANKU-Esophagus01研究也顯示，iza-bren達到OS和PFS雙重主要終點。

雙特異性ADC不再只依賴單一抗原識別腫瘤細胞，而是通過同時識別兩個腫瘤相關抗原，試圖更好地應對腫瘤異質(zhì)性、靶點表達差異和內(nèi)吞效率不足等挑戰(zhàn)。近日發(fā)表于Cancer Cell的綜述指出，雙特異性ADC可同時結合兩種不同細胞表面抗原，一方面擴大潛在患者覆蓋范圍并應對腫瘤內(nèi)異質(zhì)性，另一方面也可通過要求兩個靶點共表達來提高腫瘤選擇性，從而有望減少對正常組織的影響。該綜述還指出，近年來已有超過40款雙特異性ADC進入臨床開發(fā)，其中EGFR/HER3和EGFR/cMET是具有代表性的靶點組合。

▲常見的雙特異性ADC靶點對和進入臨床開發(fā)階段的雙特異性ADC（圖片來源：參考資料[1]）

在融資方面，雙特異性ADC也正在吸引資本支持。Sidewinder Therapeutics在4月完成1.37億美元B輪融資，用于推進下一代雙特異性ADC進入臨床開發(fā)。Sidewinder專注于開發(fā)靶向受體共復合物（receptor co-complexes）的雙特異性ADC療法。這類療法通過工程化雙特異性抗體識別由致癌驅動受體和內(nèi)吞受體組成的腫瘤特異性共復合物，從而實現(xiàn)更精準的腫瘤細胞識別與內(nèi)吞，提高藥物遞送至癌細胞的效率，同時減少對正常細胞的影響。這一融資事件顯示，雙特異性ADC不僅已經(jīng)有上市和后期臨床案例，也正在成為早期平臺公司重點布局的方向之一。

載荷和連接子創(chuàng)新，推動ADC從“遞送毒素”走向系統(tǒng)設計

下一代ADC的創(chuàng)新并不只發(fā)生在靶點端，也發(fā)生在載荷和連接子上。傳統(tǒng)ADC的載荷主要集中在微管抑制劑和拓撲異構酶I抑制劑等細胞毒性藥物，而隨著耐藥性、腫瘤異質(zhì)性和安全性挑戰(zhàn)日益受到關注，創(chuàng)新者正在探索更豐富的載荷類型、更穩(wěn)定且可控的連接子系統(tǒng)，以及更均一的偶聯(lián)方式。

例如，吉利德科學（Gilead Sciences）在2026年5月完成了對Tubulis的收購，獲得其靶向NaPi2b的抗體偶聯(lián)藥物TUB-040，以及經(jīng)過臨床驗證的Tubutecan連接子-載荷系統(tǒng)。該系統(tǒng)將拓撲異構酶I抑制劑exatecan通過基于P5偶聯(lián)技術的可裂解連接子系統(tǒng)與抗體連接，并實現(xiàn)均一的高藥物抗體比（DAR）。

今年4月，禮來（Eli Lilly and Company）宣布收購CrossBridge Bio，布局雙載荷ADC技術。CrossBridge Bio專注于開發(fā)同時遞送兩種作用機制不同載荷的ADC，以期覆蓋更多腫瘤細胞狀態(tài)并降低潛在耐藥風險。

同月，羅氏（Roche）與C4 Therapeutics圍繞抗體偶聯(lián)降解劑達成合作。根據(jù)協(xié)議，C4 Therapeutics將利用其TORPEDO平臺設計降解劑載荷，羅氏負責選擇和設計抗體，并將抗體與降解劑載荷偶聯(lián)。DAC將抗體的特異性靶向遞送能力與降解劑載荷的催化作用機制相結合，有望將蛋白降解作用更精準地引導至特定腫瘤細胞或組織中，并為高活性降解劑載荷提供更具選擇性的遞送方式。

從產(chǎn)業(yè)化開發(fā)角度看，連接子、載荷和偶聯(lián)相關小分子模塊的設計與制備，是ADC能否從分子構想走向可開發(fā)候選藥物的關鍵基礎。隨著ADC結構日益復雜，研發(fā)端不僅需要更多可選擇的連接子和載荷類型，也需要能夠支持快速合成、結構確證、純化放大和高活性載荷安全處理的一體化平臺。

藥明康德研發(fā)化學服務部構建了覆蓋連接子與載荷合成、分析及純化的一體化技術平臺，為ADC關鍵小分子組件開發(fā)提供系統(tǒng)化支持。依托超過10年的項目經(jīng)驗與580余名專業(yè)化學家團隊，RCS已累計交付超過27000種相關化合物，在多類型連接子合成方面積累了豐富實踐經(jīng)驗。平臺采用模塊化設計理念，建立了包含1000余種連接子、30多類抗體連接位點及超過30種新型載荷及其類似物的可定制化體系。

在載荷與構建模塊方面，RCS覆蓋多類主流細胞毒性分子體系，包括camptothecin類、auristatin類、maytansinoid類、PBD及duocarmycin類等，并建立了完善的構建模塊庫與快速物料調(diào)用體系，實現(xiàn)從倉儲到實驗室小于4小時的高效響應。同時，平臺支持毫克級至百克級的靈活合成規(guī)模，可滿足不同階段項目需求。配套的先進分析與分離能力涵蓋LC-MS/HPLC、CAD/ELSD檢測、高場核磁（400/500 MHz）、Prep-HPLC-MS及Prep-SFC-MS等技術，可針對穩(wěn)定性差、紫外響應弱或分離困難的連接子及載荷分子開發(fā)專用純化方案，確保結構確證與高回收率。

此外，RCS配備符合規(guī)范的高活性化合物操作實驗室，通過隔離器系統(tǒng)、嚴格去污染流程及完善的人員防護與廢棄物管理體系，實現(xiàn)高毒性載荷的安全合規(guī)處理。通過將模塊化化學設計、規(guī)模化合成能力與高標準安全體系相結合，RCS能夠幫助合作伙伴高效推進ADC連接子與載荷開發(fā)，加速創(chuàng)新偶聯(lián)療法從早期研究邁向可開發(fā)階段。

放射性核素偶聯(lián)藥物融資活躍

ADC之外，放射性核素偶聯(lián)藥物也成為2026年第二季度偶聯(lián)藥物融資中的重要亮點。輻聯(lián)科技（Full-Life Technologies）在5月完成1.5億美元融資，包括約1.1億美元D輪股權融資和4000萬美元債權融資。公司表示，資金將用于推進臨床階段放射性治療項目，包括針對前列腺癌的潛在“best-in-class”藥物[225Ac]Ac-FL-020，以及針對多種實體瘤適應癥的潛在“first-in-class”藥物[225Ac]Ac-FL-261，并支持GMP級別錒-225制造能力建設。

NUCLIDIUM在5月完成2600萬瑞士法郎B輪擴展融資，使B輪融資總額達到1.05億瑞士法郎，融資將支持NU101和NU201等銅同位素診療一體化項目的臨床開發(fā)。晶核生物（Bivision Pharmaceuticals）也在5月完成近4億元人民幣B輪融資，繼續(xù)推進診療一體化靶向放射性藥物開發(fā)。

Cellectar Biosciences在5月宣布完成最高1.4億美元融資，用于支持iopofosine I 131等項目推進。Cellectar Biosciences利用其專有的磷脂藥物偶聯(lián)物（phospholipid drug conjugate）遞送平臺，開發(fā)下一代靶向癌細胞的治療方法，通過減少脫靶效應實現(xiàn)更優(yōu)療效和更佳安全性。其在研療法iopofosine I 131旨在實現(xiàn)碘-131的靶向遞送。Iopofosine I 131正在2b期試驗中接受評估，用于治療復發(fā)或難治性華氏巨球蛋白血癥、復發(fā)或難治性多發(fā)性骨髓瘤和中樞神經(jīng)系統(tǒng)淋巴瘤。FDA已授予iopofosine I 131突破性療法認定、6項孤兒藥資格、4項罕見兒科疾病認定和2項快速通道資格，覆蓋多種癌癥適應癥。

從ADC走向一線治療，到雙特異性ADC、雙載荷ADC和RDC加速布局，偶聯(lián)藥物正在進入一個更加復雜也更具想象力的新階段。未來，這一領域的發(fā)展不僅取決于靶點和載荷選擇，也取決于能否把發(fā)現(xiàn)、設計、偶聯(lián)、DMPK、生物分析和CMC開發(fā)整合為高效協(xié)同的開發(fā)體系。藥明康德將持續(xù)依托其一體化、端到端的CRDMO平臺，助力全球合作伙伴加速推進更多創(chuàng)新偶聯(lián)藥物，為患者帶來更精準、更有效的治療選擇。

Q2 2026 Review of Conjugated Therapeutics

Conjugated therapeutics are designed by linking antibodies, peptides, small molecules, or other targeting ligands with functional payloads, enabling therapeutic agents to be delivered to specific cells, tissues, or disease microenvironments. In the second quarter of 2026, the field continued to advance rapidly. Multiple antibody-drug conjugates (ADCs) achieved important regulatory milestones, further expanding into first-line treatment, early disease management, and rare tumor settings. The first bispecific ADC was approved and delivered positive late-stage clinical results in indications including triple-negative breast cancer and esophageal squamous cell carcinoma, suggesting that dual-antigen recognition strategies are entering a more mature stage of clinical development. At the same time, mergers, acquisitions, and collaborations around novel payloads, linkers, dual-payload ADCs, and degrader-antibody conjugates (DACs) remained active, while financing for radionuclide drug conjugates (RDCs) also gained momentum. Together, these developments show that innovation in conjugated therapeutics is expanding beyond traditional ADCs toward a broader range of targeted delivery platforms.

In this evolution, linkers and payloads are among the key factors that determine whether an ADC can progress from molecular concept to developable drug candidate. WuXi AppTec Research Chemistry Services (RCS) has established a comprehensive ADC linker-payload synthesis platform, designed to support the growing demand for highly specialized cytotoxic conjugation components in next-generation targeted therapies. With more than 10 years of project experience, a team of more than 580 professional chemists, and a customizable system that includes more than 1,000 linkers, more than 30 types of antibody conjugation sites, and more than 30 novel payloads and their analogs, RCS can help partners efficiently advance ADC linker and payload development and accelerate the creation of innovative conjugate therapeutics with enhanced efficiency and confidence.

ADCs Move Toward First-Line Treatment and Early Disease Management

In the second quarter of 2026, multiple ADCs continued to move into first-line and earlier treatment settings. In May, the U.S. FDA approved Datroway (datopotamab deruxtecan), jointly developed by AstraZeneca and Daiichi Sankyo, for the treatment of adults with unresectable or metastatic triple-negative breast cancer (TNBC) who are not candidates for PD-1/PD-L1 inhibitor therapy. Datroway is a TROP2-directed ADC.

Only one month later, another TROP2-directed ADC achieved important regulatory progress in first-line TNBC. In June, the U.S. FDA approved Trodelvy (sacituzumab govitecan) for two first-line TNBC indications: as monotherapy for adults with unresectable locally advanced or metastatic TNBC who are not candidates for PD-1/PD-L1 inhibitor therapy; and in combination with Keytruda (pembrolizumab) or Keytruda Qlex for adults with unresectable locally advanced or metastatic TNBC whose tumors express PD-L1 with CPS≥10 and who are eligible for immunotherapy. Clinical trial data showed that in the ASCENT-03 study, median progression-free survival (PFS) was 9.7 months in the Trodelvy monotherapy group and 6.9 months in the chemotherapy control group. In the ASCENT-04/KEYNOTE-D19 study, median PFS was 11.2 months in the Trodelvy plus Keytruda group and 7.8 months in the control group.

The regulatory progress of Datroway and Trodelvy in first-line TNBC shows that ADCs are no longer only supplemental options after multiple lines of therapy. Instead, they are beginning to influence first-line treatment decisions alongside chemotherapy, immunotherapy, and other standard approaches. In particular, the approval of Trodelvy in combination with Keytruda highlights the growing importance of ADC and immune checkpoint inhibitor combinations. ADCs can induce tumor cell death by delivering cytotoxic payloads in a targeted manner, while immunotherapy can activate antitumor immune responses. Together, these complementary mechanisms may bring deeper and more durable disease control to some patients.

Beyond first-line treatment for advanced cancer, ADCs are also expanding into early disease management. In May, Enhertu (trastuzumab deruxtecan) received U.S. FDA approval for two new indications in HER2-positive early breast cancer, including use as neoadjuvant and adjuvant therapy for different types of early HER2-positive breast cancer.

This progress is highly significant. For many years, ADCs were used primarily in patients with advanced, recurrent, or refractory tumors. As ADCs enter neoadjuvant and adjuvant treatment settings, their value is no longer limited to delaying disease progression in advanced cancer. They may also play a role in curative-intent treatment strategies for early-stage disease.

ADCs also made regulatory progress in rare hematologic malignancies. In May, the U.S. FDA approved Decnupaz (pivekimab sunirine), developed by AbbVie, for the treatment of adult patients with blastic plasmacytoid dendritic cell neoplasm (BPDCN). Decnupaz is a CD123-directed antibody-drug conjugate.

Bispecific ADCs Receive Their First Regulatory Approval, with Clinical Pipelines Accelerating

As ADCs move into broader clinical applications, bispecific ADCs also achieved important progress in the second quarter of 2026. In June, China’s National Medical Products Administration (NMPA) approved izalontamab brengitecan, developed by Baili Tianheng, for the treatment of patients with recurrent or metastatic nasopharyngeal carcinoma. Izalontamab brengitecan simultaneously targets EGFR and HER3 and is the first bispecific ADC to receive regulatory approval. Bristol Myers Squibb has entered into a collaboration with SystImmune, a subsidiary of Baili Tianheng, to jointly develop this drug.

At the 2026 American Society of Clinical Oncology (ASCO) Annual Meeting, Bristol Myers Squibb and Baili Tianheng announced positive results from two Phase 3 clinical trials of iza-bren. In patients with previously treated unresectable locally advanced or metastatic TNBC, the PANKU-Breast02 study showed that iza-bren significantly improved overall survival (OS) and PFS compared with physician’s choice of chemotherapy. In patients with recurrent or metastatic esophageal squamous cell carcinoma, the PANKU-Esophagus01 study also showed that iza-bren met the dual primary endpoints of OS and PFS.

The rationale for bispecific ADCs is increasingly clear: they do not rely on a single antigen to recognize tumor cells. Instead, by recognizing two tumor-associated antigens simultaneously, they are designed to better address challenges such as tumor heterogeneity, variable target expression, and insufficient internalization efficiency. A recent review published in Cancer Cell noted that bispecific ADCs can bind two different cell-surface antigens at the same time. On one hand, this may broaden the potential patient population and help address intratumoral heterogeneity. On the other hand, by requiring co-expression of two targets, bispecific ADCs may improve tumor selectivity and potentially reduce effects on normal tissues. The review also noted that more than 40 bispecific ADCs have entered clinical development in recent years, with EGFR/HER3 and EGFR/cMET representing notable target combinations.

▲Common bispecific ADC target pairs and bispecific ADCs that have entered clinical development (Image source: Reference [1])

Investor interest is also building around bispecific ADCs. In April, Sidewinder Therapeutics completed a $137 million Series B financing to advance next-generation bispecific ADCs into clinical development. Sidewinder focuses on bispecific ADC therapies that target receptor co-complexes. These therapies use engineered bispecific antibodies to recognize tumor-specific co-complexes composed of oncogenic driver receptors and internalizing receptors, enabling more precise tumor cell recognition and internalization, improving drug delivery to cancer cells while reducing effects on normal cells. This financing event shows that bispecific ADCs not only have regulatory and late-stage clinical examples, but are also becoming an important area of focus for early-stage platform companies.

Payload and Linker Innovation Drives ADCs from “Toxin Delivery” Toward Systematic Design

Innovation in next-generation ADCs is taking place not only at the target level, but also in payloads and linkers. Traditional ADC payloads have mainly focused on cytotoxic agents such as microtubule inhibitors and topoisomerase I inhibitors. As drug resistance, tumor heterogeneity, and safety challenges attract increasing attention, innovators are exploring a broader range of payload types, more stable and controllable linker systems, and more homogeneous conjugation methods.

One example is Gilead Sciences’ acquisition of Tubulis in May 2026. Through the acquisition, Gilead obtained TUB-040, a NaPi2b-targeted ADC, as well as Tubutecan, a clinically validated linker-payload system. This system connects the topoisomerase I inhibitor exatecan to antibodies through a cleavable linker system based on P5 conjugation technology and achieves a homogeneous high drug-to-antibody ratio (DAR).

In April, Eli Lilly and Company announced its acquisition of CrossBridge Bio to expand into dual-payload ADC technology. CrossBridge Bio focuses on developing ADCs that deliver two payloads with different mechanisms of action simultaneously, with the goal of covering more tumor cell states and reducing potential resistance risk.

In the same month, Roche and C4 Therapeutics entered into a collaboration around antibody-degrader conjugates. Under the agreement, C4 Therapeutics will use its TORPEDO platform to design degrader payloads, while Roche will be responsible for selecting and designing antibodies and conjugating them with degrader payloads. DACs combine the targeted delivery capability of antibodies with the catalytic mechanism of degrader payloads, potentially directing protein degradation more precisely to specific tumor cells or tissues and providing a more selective delivery approach for highly active degrader payloads.

From an industrial development perspective, the design and preparation of linkers, payloads, and conjugation-related small-molecule modules are critical foundations for advancing ADCs from molecular concept to developable drug candidates. As ADC structures become increasingly complex, R&D teams need not only more linker and payload options, but also an integrated platform that can support rapid synthesis, structural confirmation, purification and scale-up, and safe handling of highly active payloads.

WuXi AppTec Research Chemistry Services (RCS) has established a comprehensive antibody–drug conjugate (ADC) linker-payload synthesis platform, designed to support the growing demand for highly specialized cytotoxic conjugation components in next-generation targeted therapies. Built upon more than a decade of experience in complex small-molecule and high-potency chemistry, the platform integrates customized linker-payload synthesis, analytical characterization, and safe handling capabilities into a flexible and scalable workflow. Supported by a team of over 580 experienced chemists, RCS has delivered more than 27,000 compounds and accumulated extensive expertise across diverse linker-payload chemistries, enabling partners to efficiently advance ADC programs from early discovery through development. The platform provides access to a highly modular linker–payload toolbox comprising over 1,000 linkers, more than 30 antibody attachment sites, and over 30 novel payloads and analogs.

RCS supports a broad spectrum of cytotoxic payload classes, including camptothecins, auristatins, maytansinoids, pyrrolobenzodiazepines (PBD), and duocarmycins, alongside a well-established modular building-block warehousing system featuring hundreds of linker and payload intermediates. This infrastructure allows rapid material supply, often transferring compounds from warehouse to laboratory within 4 hours. Meanwhile, the RCS platform support synthesis scales ranging from milligrams to hundreds of grams, facilitated by advanced analytical and purification capabilities, including LC-MS/HPLC, CAD/ELSD detection, high-field NMR, Prep-HPLC-MS, and Prep-SFC-MS. These tools enable efficient impurity identification, challenging separations, and precise structural validation, particularly for unstable or weakly UV-active linker-payload molecules.

Complementing technical expertise, RCS has dedicated high-potency laboratories equipped with isolators, strict containment protocols, and comprehensive personnel protection procedures to ensure safe and compliant handling of cytotoxic compounds. By combining modular chemistry design, scalable synthesis, advanced analytics, and robust safety infrastructure, WuXi AppTec RCS provides partners with an integrated and reliable solution for ADC linker-payload development, accelerating the creation of innovative conjugate therapeutics with enhanced efficiency and confidence.

Financing for Radionuclide Drug Conjugates Remains Active

Beyond ADCs, radionuclide drug conjugates also attracted significant investor interests in the second quarter of 2026. Full-Life Technologies completed $150 million in financing in May, including approximately $109 million in Series D equity financing and $41 million in debt financing. The company said the funds will be used to advance clinical-stage radiotherapeutic programs, including [225Ac]Ac-FL-020, a potential “best-in-class” drug for prostate cancer, and [225Ac]Ac-FL-261, a potential “first-in-class” drug for multiple solid tumor indications, while also supporting GMP-grade actinium-225 manufacturing capabilities.

NUCLIDIUM completed a CHF 26 million Series B extension in May, bringing the total Series B financing to CHF 105 million. The financing will support the clinical development of copper isotope radiotheranostics programs such as NU101 and NU201. Bivision Pharmaceuticals also completed a nearly RMB 400 million Series B financing in May to continue advancing the development of targeted radiopharmaceuticals for integrated diagnosis and treatment.

Cellectar Biosciences announced in May that it had completed financing of up to $140 million to support the advancement of programs such as iopofosine I 131. Cellectar Biosciences uses its proprietary phospholipid drug conjugate delivery platform to develop next-generation therapies targeting cancer cells, with the goal of achieving improved efficacy and safety by reducing off-target effects. Its investigational therapy iopofosine I 131 is designed to enable targeted delivery of iodine-131. Iopofosine I 131 is being evaluated in a Phase 2b trial for the treatment of relapsed or refractory Waldenstr?m macroglobulinemia, relapsed or refractory multiple myeloma, and central nervous system lymphoma. The FDA has granted iopofosine I 131 breakthrough therapy designation, 6 orphan drug designations, 4 rare pediatric disease designations, and 2 fast track designations across multiple cancer indications.

From ADCs moving into first-line treatment, to the accelerated development of bispecific ADCs, dual-payload ADCs, and RDCs, conjugated therapeutics are entering a new stage that is both more complex and more expansive. In the future, the development of this field will depend not only on target and payload selection, but also on whether discovery, design, conjugation, DMPK, bioanalysis, and CMC development can be integrated into an efficient and coordinated development system. WuXi AppTec will continue to leverage its integrated, end-to-end CRDMO platform to help global partners accelerate the development of more innovative conjugated therapeutics and bring more precise and effective therapies to patients.

參考資料：

[1] Pistilli et al., (2026). Antibody-drug conjugates in precision oncology. Cancer Cell, https://doi.org/10.1016/j.ccell.2026.05.004

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